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A mild and practical Pd/ Xiang-Phos -catalyzed enantioselective intermolecular carboheterofunctionalization reaction of 2,3-dihydrofurans is developed, leading to various optically active fused furoindolines and tetrahydrofurobenzofurans. The key to this transformation is employing two newly modified N -Me-Xiang-Phos ligands (( S , R  S )-  N -Me-X4 / X5 ) as chiral ligands under mild conditions. Moreover, this synthetic methodology can be efficiently applied to a variety of complex polysubstituted heterocycles with high chemo-, regio-, and enantio-selectivities via introducing diverse substituents on furan rings, which were hard to access by other routes.

Pd/Xiang-Phos-catalyzed enantioselective intermolecular carboheterofunctionalization under mild conditions